产品
编 号：F445024
分子式：C18H21F2N5O4S
分子量：441.45
分子式：C18H21F2N5O4S
分子量：441.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 741713-40-6
产品详情
生物活性：
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
体内研究：
R547 具有显著的体内疗效，每日口服和每周静脉注射一次。 R547 抑制肿瘤中视网膜母细胞瘤蛋白的磷酸化。Animal Model:13-14 weeks old female immunodeficient nude mice (23-25 g), with HCT116/H460a/MDA-MB-435/DU145/LOX/A549 cells xenograft
Dosage:40 mg/kg
Administration:Oral administration; daily; for 3-weeks
Result:Showed antitumor activity in all of the models in this study.
体外研究：
R547 有效抑制 CDK1/细胞周期蛋白 B、CDK2/细胞周期蛋白 E 和 CDK4/细胞周期蛋白 D1 (Ki=1-3 nM)，并且对细胞中 >120 种不相关的激酶无活性 (Ki> 5,000 nM)。 R547 有效抑制肿瘤细胞系的增殖，不受多药耐药状态、组织学类型、视网膜母细胞瘤蛋白或 p53 状态的影响，IC50 R547 相关抗体:Cell Cytotoxicity AssayCell Line:Human tumor cell lines (MDA-MB-468, MDA-MB-435, MCF-7, HCT116, SW480, RKO, HT-29, HCT15, H460a, C33A, DU145, OSA-CL, LOX, JEKO-1, REC-1)
Concentration:MTT assay
Incubation Time:5 days
Result:Has potent in vitro antiproliferative activity.
Cell Cycle AnalysisCell Line:R547, HCT116
Concentration:0.1 μM, 0.2 μM, 0.6 μM
Incubation Time:20 hours
Result:Decrease in BrdUrd incorporation and in percentage S phase in a dose-dependent, indicative of a cell cycle block in G1-S plus G2-M.
Western Blot AnalysisCell Line:HCT116 cells
Concentration:0.1 μM, 0.2 μM, 0.6 μM
Incubation Time:24 hours, 48 hours, 72 hours
Result:Showed a band corresponding to a p48/retinoblastoma fragment that becomes more intense at 48 and 72 hours.
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
体内研究：
R547 具有显著的体内疗效，每日口服和每周静脉注射一次。 R547 抑制肿瘤中视网膜母细胞瘤蛋白的磷酸化。Animal Model:13-14 weeks old female immunodeficient nude mice (23-25 g), with HCT116/H460a/MDA-MB-435/DU145/LOX/A549 cells xenograft
Dosage:40 mg/kg
Administration:Oral administration; daily; for 3-weeks
Result:Showed antitumor activity in all of the models in this study.
体外研究：
R547 有效抑制 CDK1/细胞周期蛋白 B、CDK2/细胞周期蛋白 E 和 CDK4/细胞周期蛋白 D1 (Ki=1-3 nM)，并且对细胞中 >120 种不相关的激酶无活性 (Ki> 5,000 nM)。 R547 有效抑制肿瘤细胞系的增殖，不受多药耐药状态、组织学类型、视网膜母细胞瘤蛋白或 p53 状态的影响，IC50 R547 相关抗体:Cell Cytotoxicity AssayCell Line:Human tumor cell lines (MDA-MB-468, MDA-MB-435, MCF-7, HCT116, SW480, RKO, HT-29, HCT15, H460a, C33A, DU145, OSA-CL, LOX, JEKO-1, REC-1)
Concentration:MTT assay
Incubation Time:5 days
Result:Has potent in vitro antiproliferative activity.
Cell Cycle AnalysisCell Line:R547, HCT116
Concentration:0.1 μM, 0.2 μM, 0.6 μM
Incubation Time:20 hours
Result:Decrease in BrdUrd incorporation and in percentage S phase in a dose-dependent, indicative of a cell cycle block in G1-S plus G2-M.
Western Blot AnalysisCell Line:HCT116 cells
Concentration:0.1 μM, 0.2 μM, 0.6 μM
Incubation Time:24 hours, 48 hours, 72 hours
Result:Showed a band corresponding to a p48/retinoblastoma fragment that becomes more intense at 48 and 72 hours.
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